DP 4978
LY3009120
CAS: 1454682-72-4
Molecular Formula: C23H29FN6O
DP 4978 - Names and Identifiers
DP 4978 - Physico-chemical Properties
| Molecular Formula | C23H29FN6O |
| Molar Mass | 424.51 |
| Density | 1?+-.0.06 g/cm3(Predicted) |
| Solubility | DMSO : ≥ 38 mg/mL (89.51 mM) |
| pKa | 13.52±0.70(Predicted) |
| Storage Condition | -20℃ |
| Use | LY3009120 is a pan-RAF inhibitor, which inhibits BRAFV600E,BRAFWT and CRAWT with IC50 of 5.8,9.1 and 15 nM, respectively. |
| In vitro study | LY3009120 inhibited the growth of A375 and HCT116 cells with an IC50 of 9.2 and 220 μm, respectively. LY3009120 inhibits the tyrosine kinase KDR with an IC50 of 3.9 μm. |
| In vivo study | LY3009120 (15 or 30 mg/kg, p.o.) dose-dependently inhibited tumor growth in rats bearing BRAF V600E ST019VR PDX tumors. In nude mice bearing A375 xenografts, LY3009120 (3 to 50 mg/kg, p.o.) single dose of oral treatment dose-dependent inhibition of phosphate-ERK,4.36 mg/kg dose inhibition of 50% phosphate-ERK (EC50),68.9 inhibition of phospho-ERK (EC50) was achieved at 165 ng/mL or 50% nM plasma concentration. |
DP 4978 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.356 ml | 11.778 ml | 23.556 ml |
| 5 mM | 0.471 ml | 2.356 ml | 4.711 ml |
| 10 mM | 0.236 ml | 1.178 ml | 2.356 ml |
| 5 mM | 0.047 ml | 0.236 ml | 0.471 ml |
Last Update：2024-01-02 23:10:35
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